Description |
SH-4-54 is a most potent, small molecule, nonphosphorylated STAT inhibitor, with KDs of 300, 464 nM for STAT3 and STAT5, respectively.
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Target |
STAT3:300 nM (Kd)
STAT5:464 nM (Kd)
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In Vitro |
SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations.SH-4-54 shows unprecedented cytotoxicity in human BTSCs, displays no toxicity in human fetal astrocytes, potently suppresses pSTAT3 with nanomolar IC50s, inhibiting STAT3's downstream targets, and shows no discernible off-target effects at therapeutic doses[1].
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In Vivo |
SH-4-54 exhibits blood-brain barrier permeability potently controls glioma tumor growth, and inhibits pSTAT3 in vivo. SH-4-54 demonstrates the power of STAT3 inhibitors for the treatment of BTSCs and validates the therapeutic efficacy of a STAT3 inhibitor for GBM clinical application.SH-4-54 decreases pSTAT3 expression in tumor cells of treated mice. SH-4-54 appears to decrease proliferation and increase apoptosis of treated tumors[1].
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Density | 1.431±0.06 g/cm3 |
Boiling Point | 717.2±70.0 °C at 760 mmHg |
Flash Point | 387.5±35.7 °C |
Exact Mass | 610.156067 |
PSA | 103.37000 |
LogP | 7.64 |
Vapour Pressure | 0.0±2.4 mmHg at 25°C |
Storage condition | -20℃ |